An article Regioselective microwave synthesis and derivatization of 1,5-diaryl-3-amino-1,2,4-triazoles and a study of their cholinesterase inhibition properties WOS:000474266800051 published article about SOLID-PHASE SYNTHESIS; ASSISTED SYNTHESIS; ACETYLCHOLINESTERASE; DISCOVERY; 1,2,4-TRIAZOLES; DERIVATIVES; ABSORPTION; POTENT in [Santos, Sabrina Neves; de Souza, Gabriela Alves; Pereira, Thiago Moreira; Franco, Daiana Portella; Lacerda, Renata Barbosa; Kummerle, Arthur Eugen] Univ Fed Rural Rio Janeiro, Chem Inst, Mol Divers & Med Chem Lab, Lab Diversidade Mol & Quim Med LaDMol QM, BR-23989700 Seropedica, RJ, Brazil; [Santos, Sabrina Neves; de Souza, Gabriela Alves; Pereira, Thiago Moreira; Franco, Daiana Portella; Del Cistia, Catarina de Nigris; Sant’Anna, Carlos Mauricio R.; Lacerda, Renata Barbosa; Kummerle, Arthur Eugen] Univ Fed Rural Rio Janeiro, Programa Posgrad Quim PPGQ, BR-23989700 Seropedica, RJ, Brazil in 2019.0, Cited 39.0. Safety of 4-Nitrobenzoic acid. The Name is 4-Nitrobenzoic acid. Through research, I have a further understanding and discovery of 62-23-7
Herein we describe the development of an efficient one-pot regioselective synthesis protocol to obtain N-protected or N-deprotected 1,5-diaryl-3-amino-1,2,4-triazoles from N-acyl-N-Boc-carbamidothioates. This improved protocol using microwave irradiation and low reaction times (up to 1 h) furnished desired compounds in yields ranging from 50 to 84%. This chemistry is useful for a variety of aromatic groups with electronically diverse substituents. The design and correct derivation of the amino group led to compounds able to inhibit cholinesterases with good IC50 of up to 1 mu M. Also, the mode of action (mixed-type) and SAR analysis for this series of compounds was described by means of kinetic and molecular modelling evaluations, showing potential for this class of compounds as new scaffolds for this biological activity.
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Reference:
Phthalazine – Wikipedia,
,Phthalazine | C8H6N2 – PubChem